CA3236238A1 - Kras g12c inhibitors - Google Patents

Kras g12c inhibitors Download PDF

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Publication number
CA3236238A1
CA3236238A1 CA3236238A CA3236238A CA3236238A1 CA 3236238 A1 CA3236238 A1 CA 3236238A1 CA 3236238 A CA3236238 A CA 3236238A CA 3236238 A CA3236238 A CA 3236238A CA 3236238 A1 CA3236238 A1 CA 3236238A1
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CA
Canada
Prior art keywords
compound
group
substituted
halo
alkyl
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA3236238A
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English (en)
French (fr)
Inventor
Snahel PATEL
Hiroko Tanaka
Daniel A. Erlanson
Philip A. GERKEN
John C. WIDEN
Monika Jane WILLIAMS
Irina DOTSENKO
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Frontier Medicines Corp
Original Assignee
Frontier Medicines Corp
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Filing date
Publication date
Application filed by Frontier Medicines Corp filed Critical Frontier Medicines Corp
Publication of CA3236238A1 publication Critical patent/CA3236238A1/en
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA3236238A 2021-11-05 2022-11-04 Kras g12c inhibitors Pending CA3236238A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US202163276478P 2021-11-05 2021-11-05
US63/276,478 2021-11-05
US202263356906P 2022-06-29 2022-06-29
US63/356,906 2022-06-29
US202263403565P 2022-09-02 2022-09-02
US63/403,565 2022-09-02
PCT/US2022/079324 WO2023081840A1 (en) 2021-11-05 2022-11-04 Kras g12c inhibitors

Publications (1)

Publication Number Publication Date
CA3236238A1 true CA3236238A1 (en) 2023-05-11

Family

ID=84537713

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3236238A Pending CA3236238A1 (en) 2021-11-05 2022-11-04 Kras g12c inhibitors

Country Status (10)

Country Link
US (2) US20250340548A1 (https=)
EP (1) EP4426695A1 (https=)
JP (1) JP2024540410A (https=)
KR (1) KR20240114793A (https=)
AU (1) AU2022380839A1 (https=)
CA (1) CA3236238A1 (https=)
IL (1) IL312381A (https=)
MX (1) MX2024005228A (https=)
TW (1) TW202334138A (https=)
WO (1) WO2023081840A1 (https=)

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JP2025510656A (ja) * 2022-03-24 2025-04-15 ベイジーン スウィッツァーランド ゲーエムベーハー 複素環式化合物、その組成物、及びそれらを用いた治療方法
WO2023230190A1 (en) 2022-05-25 2023-11-30 Quanta Therapeutics, Inc. Pyrimidine based modulators and uses thereof
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CN119317629A (zh) * 2022-06-10 2025-01-14 百时美施贵宝公司 作为kras抑制剂的四氢吡啶并3,4-d嘧啶衍生物
WO2023246777A1 (en) * 2022-06-20 2023-12-28 Jacobio Pharmaceuticals Co., Ltd. K-ras mutant protein inhibitors
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KR20260041941A (ko) 2023-03-15 2026-03-27 콴타 테라퓨틱스, 인크. Kras 조절 인자 및 이의 용도
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
EP4705302A1 (en) * 2023-05-04 2026-03-11 Frontier Medicines Corporation Pyrido[4,3-d]pyrimidine derivatives as mutant kras g12c inhibitors for the treatment of cancer
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ras相關疾病或病症之組合療法
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2025085580A1 (en) * 2023-10-17 2025-04-24 Windermere Therapeutics, Inc. Kras(g12d) inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025179058A1 (en) 2024-02-21 2025-08-28 Frontier Medicines Corporation Pyridopyrimidine derivative as kras g12c inhibitor for the treatment of brain metastasis
WO2025188668A1 (en) 2024-03-04 2025-09-12 Frontier Medicines Corporation Combination of a kras g12c inhibitor with an immune checkpoint inhibitor for the treatment of cancer
WO2025194340A1 (en) 2024-03-19 2025-09-25 Frontier Medicines Corporation Polymorphic forms of kras inhibitors and uses thereof
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ras抑制劑
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026035945A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload
WO2026035947A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026064527A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload
WO2026064520A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

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EA202190749A1 (ru) 2018-09-10 2021-07-09 Мирати Терапьютикс, Инк. Способы комбинированной терапии
JP2022500385A (ja) 2018-09-10 2022-01-04 ミラティ セラピューティクス, インコーポレイテッド 組み合わせ療法
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CN112694475B (zh) 2019-10-23 2025-09-23 苏州泽璟生物制药股份有限公司 环烷基类和杂环烷基类抑制剂及其制备方法和应用
CN113045565A (zh) * 2019-12-27 2021-06-29 微境生物医药科技(上海)有限公司 新型K-Ras G12C抑制剂
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Also Published As

Publication number Publication date
MX2024005228A (es) 2024-07-24
WO2023081840A1 (en) 2023-05-11
EP4426695A1 (en) 2024-09-11
US12291539B2 (en) 2025-05-06
KR20240114793A (ko) 2024-07-24
US20250340548A1 (en) 2025-11-06
TW202334138A (zh) 2023-09-01
JP2024540410A (ja) 2024-10-31
IL312381A (en) 2024-06-01
AU2022380839A1 (en) 2024-06-06
US20250019387A1 (en) 2025-01-16

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